Various species from the genera Wedelia, Eclipta and Aspilia have been disclosed to have a variety of different biological or pharmacological activities.
Two frequently studied species of these genera are Wedelia calendulaceae and Eclipta alba. The most common medicinal use of extracts from these plants is for treatment of liver ailments. For this use, the active compounds found in these species are believed to be coumestans, especially wedelolactone and related compounds. Extracts from these plants have also been used to treat a number of other ailments such as catarrh, skin diseases, elephantiasis, toothaches and headaches, as well as being used as emetic and purgative materials, and as external antiseptics. Shoot extracts have been shown to have antibiotic activity against certain species. The following references disclose activities of extracts of W. calendulacea and E. alba, methods for obtaining extracts from them, and active components isolated from the extracts: Bhargava, K. K & T. R. Seshadri, "Chemistry of Medicinal Plants: Eclipta alba and Wedelia calendulacea", Journal of Research of Indian Medicine, Vol. 9, No. 1 (1974), pp. 9-15; Wagner, H., B. Geyer, Y. Kiso, H. Hikino & G. S. Rao, "Coumestans as the Main Active Principles of the Liver Drugs Eclipta alba and Wedelia calendulacea", Planta Medica, Vol. 5 (1986), pp. 370-374; Handa, S. S., P. Prakash & B. Roy, "Bioactivity Directed Extraction and Fractionation of Eclipta alba--an Antihepatotoxic Drug of Indian Origin", Indian Journal of Pharmaceutical Sciences, (Jan.-Feb., 1984), p. 50 (abstract only); Govindachari, T. R., K. Nagarajan & B. R. Pai, "Chemical Examination of Wedelia calendulacea. Part I. Structure of Wedelolactone", Journal of the Chemical Society, (1956), pp. 629-632; Govindachari, T. R., K. Nagarajan, B. R. Pai & P. C. Parthasarathy, "Chemical Investigation of Wedelia calendulacea. Part II. The Position of the Methoxyl Group in Wedelolactone", Journal of the Chemical Society, (1957), pp. 545-547; Govindachari, T. R., K. Nagarajan & P. C. Parthasarathy, "Chemical Examination of Wedelia calendulacea. Part III. Synthesis of Tri-O-methylwedelolactone", Journal of the Chemical Society, (1957), pp. 548-551; Govindachari, T. R., K. Nagarajan & P. C. Parthasarathy, "Chemical Examination of Wedelia calendulacea-IV Synthetic Analogues of Wedelolactone", Tetrahedron, Vol. 15 (1961), pp. 129-131; Govindachari, T. R. & M. S. Premila, "The Benzofuran Norwedelic Acid from Wedelia calendulacea", Phytochemistry, Vol. 24, No. 12 (1985), pp. 3068-3069; Bhargava, K. K., N. R. Krishnaswamy, & T. R. Seshadri, "Isolation of Desmethylwedelolactone & Its Glucoside from Eclipta alba", Indian Journal of Chemistry, Vol. 8 (1970), pp. 664-665; Bhargava, K. K, N. R. Krishnaswamy & T. R. Seshadri, "Desmethylwedelolactone Glucoside from Eclipta alba Leaves", Indian Journal of Chemistry, Vol 10 (Aug., 1972), pp. 810-811; Wagner, H. & B. Fessler, "In-Vitro-5-Lipoxygenasehemmung durch Eclipta alba Extrakte und das Coumestan-Derivat Wedelolacton", Planta Medica. (1986), No. 5, pp. 374-377; Krishnaswamy, N. R., T. R. Seshadri & B. R. Sharma, "The Structure of a New Polythienyl from Eclipta alba", Tetrahedron Letters, No. 35 (1966), pp. 4227-4230; and German Patent Application No. DE3,525,363 of Medice Chem.-pharm. Fabrik Putter GmbH & Co. KG, Inventor H. Wagner, published Jan. 22, 1987.
Antihepatotoxic activity has also been reported for an extract from the plant Wedelia chinensis: Yang, L. -L., K. -Y. Yen, C. Konno, Y. Oshima, Y. Kiso & H. Hikino, "Antihepatotoxic Drugs. Part 32. Antihepatotoxic Principles of Wedelia chinensis Herbs", Planta Medica (1986), No. 6, pp. 499-500. Antibacterial activity has also been discovered in extracts from other plants of the genera Wedelia. Eclipta and Aspilia: Roque, N. F., T. L. Giannella, A. M. Giesbrecht & R. Barbosa, "Kaurene Diterpenes from Wedelia paludosa", Rev. Latinoamer. Quim., Vol 18, No. 3 (1987), pp. 110-111; Farouk, A., A. K. Bashir & A. K. M. Salih, "Antimicrobial Activity of Certain Sudanese Plants used in Folkloric Medicine. Screening for Antibacterial Activity (I)", FTRPAE, Fitoterapia, Vol. 54, Issue 1 (1983), pp. 3-7; Rodriguez, E., M. Aregullin, T. Nishida, S. Uehara, R. Wrangham, Z. Abramowski, A. Finlayson & G. H. N. Towers, "Thiarubrine A, a Bioactive Constituent of Aspilia (Asteraceae) consumed by Wild Chimpanzees", Experientia, Vol. 41 (1985), pp. 419-420; and "Chimpanzees Guide Researchers to New Antibiotic", American Pharmacy, Vol. NS26, No. 3 (Mar., 1986), p. 13.
It is an object of the subject invention to provide novel compositions having mucosal-protective activity.
It is another object of the subject invention to provide novel methods for treating or preventing gastrointestinal maladies such as gastritis, non-ulcer dyspepsia, gastroesophageal reflux disease, esophagitis, gastric ulcers, duodenal ulcers, gastric cancer, Zollinger-Ellison syndrome, ethanol-induced damage, non-steroidal anti-inflammatory drug (NSAID)-induced damage, ileitis, Crohn's disease, colitis, ulcerative colitis, and inflammatory bowel disease.
It is also an object of the subject invention to provide novel processes for obtaining extracts from certain plant species having mucosal-protective activity.